Pharmaceutics | |
Preparation and Characterization of Amino Acids-Based Trimethoprim Salts | |
Amr ElShaer1  Peter Hanson1  Tony Worthington1  Peter Lambert1  | |
[1] id="af1-pharmaceutics-04-00179">Aston Pharmacy School, Aston University, Aston Triangle, Birmingham B4 7ET, | |
关键词: trimethoprim; salt formation; fourier transform infrared; 1H nuclear magnetic resonance; thermogrametric analysis; Pseudomonas aeruginosa; minimum inhibitory concentration studies; | |
DOI : 10.3390/pharmaceutics4010179 | |
来源: mdpi | |
【 摘 要 】
Trimethoprim (TMP) is a dihydrofolate reductase (DHFR) inhibitor which prevents the conversion of dihydrofolic acid into tetrahydrofolic acid, resulting in the depletion of the latter and leading to bacterial death. Oral bioavailability of TMP is hindered by both its low solubility and low permeability. This study aims to prepare novel salts of TMP using anionic amino acids; aspartic and glutamic acid as counter ions in order to improve solubility and dissolution. TMP salts were prepared by lyophilisation and characterized using FT-IR spectroscopy, proton nuclear magnetic resonance (1HNMR), Differential Scanning Calorimetry (DSC) and Thermogravimetric analysis (TGA). Both the amino acids formed salts with TMP in a 1:1 molar ratio and showed a 280 fold improvement in solubility. Investigation of the microbiological activity of the prepared salts against TMP sensitive
【 授权许可】
CC BY
© 2012 by the authors; licensee MDPI, Basel, Switzerland.
【 预 览 】
Files | Size | Format | View |
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RO202003190045626ZK.pdf | 330KB | download |